AU2003205604B8 - Process for the preparation of 7alpha-methylsteroids - Google Patents

Process for the preparation of 7alpha-methylsteroids Download PDF

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Publication number
AU2003205604B8
AU2003205604B8 AU2003205604A AU2003205604A AU2003205604B8 AU 2003205604 B8 AU2003205604 B8 AU 2003205604B8 AU 2003205604 A AU2003205604 A AU 2003205604A AU 2003205604 A AU2003205604 A AU 2003205604A AU 2003205604 B8 AU2003205604 B8 AU 2003205604B8
Authority
AU
Australia
Prior art keywords
hydroxy
methyl
steroid
copper
mmol
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired
Application number
AU2003205604A
Other languages
English (en)
Other versions
AU2003205604B2 (en
AU2003205604A1 (en
Inventor
Van P. A. M. Buggenum
M. Ostendorf
J. Stoelwinder
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme BV
Original Assignee
Merck Sharp and Dohme BV
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck Sharp and Dohme BV filed Critical Merck Sharp and Dohme BV
Publication of AU2003205604A1 publication Critical patent/AU2003205604A1/en
Assigned to N.V. ORGANON reassignment N.V. ORGANON Request for Assignment Assignors: AKZO NOBEL N.V.
Application granted granted Critical
Publication of AU2003205604B2 publication Critical patent/AU2003205604B2/en
Publication of AU2003205604B8 publication Critical patent/AU2003205604B8/en
Assigned to MSD OSS B.V. reassignment MSD OSS B.V. Request to Amend Deed and Register Assignors: N.V. ORGANON
Assigned to MERCK SHARP & DOHME B.V. reassignment MERCK SHARP & DOHME B.V. Request to Amend Deed and Register Assignors: MSD OSS B.V.
Anticipated expiration legal-status Critical
Expired legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0081—Substituted in position 17 alfa and 17 beta
    • C07J1/0085—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being a saturated hydrocarbon group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0081—Substituted in position 17 alfa and 17 beta
    • C07J1/0088—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being an unsaturated hydrocarbon group
    • C07J1/0096—Alkynyl derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C07J5/0007—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond not substituted in position 17 alfa
    • C07J5/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond not substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)
AU2003205604A 2002-01-21 2003-01-14 Process for the preparation of 7alpha-methylsteroids Expired AU2003205604B8 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP02075230.9 2002-01-21
EP02075230 2002-01-21
PCT/EP2003/000339 WO2003059931A1 (en) 2002-01-21 2003-01-14 PROCESS FOR THE PREPARATION OF 7α-METHYLSTEROIDS

Publications (3)

Publication Number Publication Date
AU2003205604A1 AU2003205604A1 (en) 2003-07-30
AU2003205604B2 AU2003205604B2 (en) 2009-11-26
AU2003205604B8 true AU2003205604B8 (en) 2009-12-24

Family

ID=8185555

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2003205604A Expired AU2003205604B8 (en) 2002-01-21 2003-01-14 Process for the preparation of 7alpha-methylsteroids

Country Status (28)

Country Link
US (2) US20050090476A1 (ja)
EP (1) EP1470151B1 (ja)
JP (1) JP5250174B2 (ja)
KR (1) KR100937179B1 (ja)
CN (1) CN100372864C (ja)
AR (1) AR038165A1 (ja)
AT (1) ATE453659T1 (ja)
AU (1) AU2003205604B8 (ja)
BR (1) BRPI0306736B8 (ja)
CA (1) CA2472379C (ja)
DE (1) DE60330749D1 (ja)
EC (1) ECSP045180A (ja)
EG (1) EG23417A (ja)
ES (1) ES2336439T3 (ja)
HR (1) HRP20040634B1 (ja)
IL (2) IL162770A0 (ja)
IS (1) IS2740B (ja)
MX (1) MXPA04007049A (ja)
NO (1) NO327095B1 (ja)
NZ (1) NZ533970A (ja)
PE (1) PE20030926A1 (ja)
PL (1) PL208163B1 (ja)
RO (1) RO122913B1 (ja)
RS (1) RS51490B (ja)
RU (1) RU2305105C2 (ja)
TW (1) TWI322813B (ja)
WO (1) WO2003059931A1 (ja)
ZA (1) ZA200405257B (ja)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10213371C1 (de) * 2002-03-21 2003-12-24 Schering Ag Verfahren zur Herstellung von 7alpha-Methylsteroiden
GB0304927D0 (en) * 2003-03-04 2003-04-09 Resolution Chemicals Ltd Process for the production of tibolone
KR100716981B1 (ko) * 2004-09-30 2007-05-10 삼성전자주식회사 대중교통의 최적경로 검색방법 및 이를 이용한 휴대용 기기
US20130123541A1 (en) * 2009-06-29 2013-05-16 Merz Pharma Gmbh & Co. Kgaa Method of preparing 3,3,5,5-tetramethylcyclohexanone
CN111944001A (zh) * 2020-07-09 2020-11-17 浙江神洲药业有限公司 一种替勃龙的制备方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3341557A (en) * 1961-06-05 1967-09-12 Upjohn Co 7-methyltestosterones
WO2000059920A2 (en) * 1999-04-06 2000-10-12 Akzo Nobel N.V. Orally active 7.alpha.-alkyl androgens
AU2001282016B2 (en) * 2000-07-28 2005-11-10 N.V. Organon 16alpha-methyl or ethyl substituted estrogens

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3470216A (en) * 1966-11-29 1969-09-30 Du Pont Selected 17,17-difluoro unsaturated androstanes
FR2054527B1 (ja) * 1969-07-28 1973-06-08 Roussel Uclaf
US3798213A (en) * 1971-01-25 1974-03-19 Merck & Co Inc 7 alpha-methyl-20-spiroxane-3-ones and process
DE2558088C2 (de) * 1975-12-19 1985-05-30 Schering AG, 1000 Berlin und 4709 Bergkamen Verfahren zur Herstellung von 4-Androsten-3,17-dion-Derivaten
JPS56145239A (en) * 1980-04-11 1981-11-11 Sumitomo Chem Co Ltd Novel bicyclooctane derivative and its preparation
US4298559A (en) * 1980-07-23 1981-11-03 Dow Corning Corporation High yield silicon carbide from alkylated or arylated pre-ceramic polymers
US6054446A (en) * 1997-12-24 2000-04-25 Sri International Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use
US6548491B2 (en) * 1997-12-24 2003-04-15 Sri International Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use
TW548277B (en) * 1999-07-16 2003-08-21 Akzo Nobel Nv Orally active androgens
HUP0203611A3 (en) * 1999-12-02 2004-07-28 Akzo Nobel Nv 14,15-beta-methylene substituted androgens and their use for preparation of the medicaments
WO2001058919A2 (en) * 2000-02-11 2001-08-16 Sri International Synthesis of anti-estrogenic and other therapeutic steroids from 21-hydroxy-19-norpregna-4-en-3-one
US20040010138A1 (en) * 2002-03-21 2004-01-15 Schering Ag Process for the production of 7alpha-methyl steroids
US7304157B2 (en) * 2004-09-28 2007-12-04 Bristol-Myers Squibb Company Efficient synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3341557A (en) * 1961-06-05 1967-09-12 Upjohn Co 7-methyltestosterones
WO2000059920A2 (en) * 1999-04-06 2000-10-12 Akzo Nobel N.V. Orally active 7.alpha.-alkyl androgens
AU2001282016B2 (en) * 2000-07-28 2005-11-10 N.V. Organon 16alpha-methyl or ethyl substituted estrogens

Also Published As

Publication number Publication date
IL162770A (en) 2011-06-30
EP1470151B1 (en) 2009-12-30
DE60330749D1 (de) 2010-02-11
KR20040077727A (ko) 2004-09-06
ZA200405257B (en) 2005-08-31
BRPI0306736B1 (pt) 2017-11-07
MXPA04007049A (es) 2004-10-14
AR038165A1 (es) 2004-12-29
RU2305105C2 (ru) 2007-08-27
ATE453659T1 (de) 2010-01-15
JP5250174B2 (ja) 2013-07-31
YU63004A (sh) 2006-08-17
IS2740B (is) 2011-06-15
PL371583A1 (en) 2005-06-27
CN1863814A (zh) 2006-11-15
ES2336439T3 (es) 2010-04-13
HRP20040634B1 (hr) 2013-07-31
AU2003205604B2 (en) 2009-11-26
AU2003205604A1 (en) 2003-07-30
RU2004125580A (ru) 2006-01-27
PE20030926A1 (es) 2003-10-29
NO20043455L (no) 2004-08-19
BRPI0306736B8 (pt) 2021-05-25
RS51490B (sr) 2011-04-30
PL208163B1 (pl) 2011-03-31
EG23417A (en) 2005-06-28
HRP20040634A2 (en) 2004-10-31
US20050090476A1 (en) 2005-04-28
CA2472379C (en) 2010-05-25
BR0306736A (pt) 2004-12-28
ECSP045180A (es) 2004-08-27
RO122913B1 (ro) 2010-04-30
JP2005519899A (ja) 2005-07-07
EP1470151A1 (en) 2004-10-27
CN100372864C (zh) 2008-03-05
NO327095B1 (no) 2009-04-20
TWI322813B (en) 2010-04-01
CA2472379A1 (en) 2003-07-24
TW200302731A (en) 2003-08-16
WO2003059931A1 (en) 2003-07-24
NZ533970A (en) 2005-10-28
IL162770A0 (en) 2005-11-20
IS7339A (is) 2004-06-28
KR100937179B1 (ko) 2010-01-19
US20100204497A1 (en) 2010-08-12

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Legal Events

Date Code Title Description
PC1 Assignment before grant (sect. 113)

Owner name: N.V. ORGANON

Free format text: FORMER APPLICANT(S): AKZO NOBEL N.V.

TH Corrigenda

Free format text: IN VOL 23, NO 46, PAGE(S) 11224 UNDER THE HEADING APPLICATIONS ACCEPTED - NAME INDEX UNDER THE NAME N.V. ORGANON, APPLICATION NO. 2003205604, UNDER INID (72), CORRECT THE CO-INVENTOR TO BUGGENUM, VAN P. A. M.

FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired